This invention relates to new prostacyclin derivatives and their alkali addition salts, a method of their synthesis and use for medicals.
It is said that prostacyclin is unstable and has wide divergent and systemic biological activities.
Therefore, stable prostacyclin analogues having selective biological effects are desired for medical use.
Prostacyclin (PGI.sub.2) is known to have an action of anti-thrombotics, vasodilatives or anti-ulceratives. ##STR3##
Oxygen atom between 6,9 positions is chemically unstable and therefore more stable prostacyclin analogues are investigated.
In the aforesaid formula of prostacyclin, prostacyclin analogues having oxygen atom at 6,9-position (--O--) replaced by carbon atom (--CH.sub.2 --), are synthesized (Stanley M. Roberts & Feodor Scheinmann Eds.; New Synthetic Routes of Prostaglandins and Thromboxanes, Academic Press (1982), 221-31p.).
Moreovre, it is known that prostaglandin analogues are dehydrogenated to 15-ketoprostaglandin by 15-hydroxyprostaglandin dehydrogenase to lose their activities. (Jarabak J. and Braithwaite S. S.; Arch. Biochem. Biophys. (1976), 177-245p.). By introducing a triple fond (--C.tbd.C--) at 13 position, prostaglanedins can be stabilized from inactivation due to 15-hydroxyprostaglandin dehydrogenase. (Josef Fried, D. K. Mitra, M. Nagarajan & M. M. Mohrotra; J. Med. Chem. 23, 234-7p. (1980)).